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Title: Synthesis and structure-activity relationship of 2-thiopyrimidine-4-one analogs as antimicrobial and anticancer agents
Authors: Supaluk Prachayasittikul
Apilak Worachartcheewan
Chanin Nantasenamat
Maneekarn Chinworrungsee
Nirun Sornsongkhram
Somsak Ruchirawat
Virapong Prachayasittikul
Srinakharinwirot University
Mahidol University
Chulabhorn Research Institute
Keywords: Chemistry;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Feb-2011
Citation: European Journal of Medicinal Chemistry. Vol.46, No.2 (2011), 738-742
Abstract: Considering that some thiopyrimidines were previously reported as potential therapeutics, the present study achieved novel analogs of bioactive 2-substituted thiopyrimidines-4-(3H)-ones via base catalyzed alkylation reaction of 2-thiouracil using alkyl and aralkyl bromides. The title compounds were 2-(1-butylthio)pyrimidine-4(3H)-one (5a), 2-(2-butylthio)pyrimidine-4(3H)-one (5b), 2-(cyclohexylmethylthio)pyrimidine-4(3H)-one (5c), 2-(benzylthio) pyrimidine-4(3H)-one (5d) and 2-(1-adamantylthio)pyrimidine-4(3H)-one (5e). Bioactivity tests revealed that thiopyrimidines 5a, 5c, 5d and 5e exhibited antimicrobial activity. The thiopyrimidine-4-one (5c) showed complete inhibition against Streptococcus pyogenes and Branhamella catarrhalis as well as antifungal action against Candida albicans. Significantly, the 1-adamantylthiopyrimidine (5e) was shown to be the most potent cytotoxic compound against multidrug-resistant small cell lung cancer (H69AR). Their structure-activity relationships were discussed. © 2010 Elsevier Masson SAS. All rights reserved.
ISSN: 17683254
Appears in Collections:Scopus 2011-2015

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